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Design and development of Nrf2 modulators for cancer chemoprevention and therapy: a review

Matej Sova1, Luciano Saso2

  • 1Faculty of Pharmacy, University of Ljubljana, Ljubljana, Slovenia, matej.sova@ffa.uni-lj.si.

Drug Design, Development and Therapy
|October 6, 2018
PubMed

Insights

The Nrf2/Keap1 pathway protects cells from stress and is crucial for cancer therapy. This review details Nrf2 modulators, activators, and inhibitors for cancer chemoprevention and treatment.

Area of Science:

  • Biochemistry
  • Cell Biology
  • Molecular Biology

Background:

  • The Nuclear factor erythroid 2-related factor 2 (Nrf2)/Kelch-like ECH-associated protein 1 (Keap1) pathway is a critical cellular defense against oxidative and xenobiotic stress.
  • This pathway regulates the expression of numerous cytoprotective and detoxifying enzymes, maintaining cellular redox homeostasis.
  • Dysregulation of Nrf2 activity is implicated in various diseases, notably cancer.

Purpose of the Study:

  • To review design strategies for developing Nrf2 modulators.
  • To highlight recent advancements in Nrf2 activators and inhibitors.
  • To discuss the potential of Nrf2 modulators in cancer chemoprevention and therapy.

Main Methods:

  • Literature review of Nrf2/Keap1 pathway research.
  • Analysis of design strategies for Nrf2 modulators.
  • Summary of in vitro and in vivo studies on Nrf2 activators and inhibitors.

Main Results:

  • Detailed description of various design strategies for Nrf2 modulators.
  • Identification of key Nrf2 activators and inhibitors with recent development.
  • Compilation of evidence from in vitro and in vivo studies.

Conclusions:

  • Targeting the Nrf2 pathway offers a promising strategy for cancer chemoprevention and treatment.
  • Nrf2 modulators, including activators and inhibitors, show potential as therapeutic agents.
  • Further research into Nrf2 modulators could lead to novel cancer therapies.
Keywords:
Nrf2cancer therapeuticschemopreventive agentscytoprotectiveoxidative stresssignaling pathway

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